Table 1

Summary of results obtained with avermectin analogs when tested against pentylenetetrazole-induced (120 mg/kg, i.p.) seizures and on Rotarod performance in the mouse

L-NumberCompoundPTZ Mouse ED50Rotarod Mouse MEDLD50 Mouse
mg/kg, i.p.
Diazepam0.263
L-676,893AVM A2a0.48>2.513.5
L-751,53123-Oxo-AVM A2a0.4928
L-642,12623-Oxo-AVM B2a1.1<32
L-652,26423-Methyl-AVM B2a2.6>6<<100
L-676,897AVM B2a2.7>6.050
L-676,891AVM A1a4.625
L-669,437Nemadectin7.2>4064
L-701,023Doramectin7.2
L-708,38123-Gem-difluoro-IVM9.1>40
L-734,8734a-O-MEM-22,23-dihydro-AVM B111.9>40
L-759,1545-MeO-Nemadectin12.7
L-759,5365-MeO-Doramectin13.8
L-676,863Abamectin (AVM B1a)20.5>7526
L-638,72522,23-Dihydro-AVM A1a21.2>80
L-693,75213-Epi-avermectin B1a24.8160
L-640,471IVM28.2>30026
L-694,55413-Epi-O-MOM-AVM B1a aglycone34.1>160
L-656,7484"-Deoxy-4"-epi-methylamino-AVM B1a34.633
L-697,96013-Epi-O-MOM-AVM B2a aglycone37.9>80310
L-653,43313-β-chloro-13-desoxy-ivermectin aglycone43.3>180
L-676,913AVM B1a aglycone43.9>50
L-697,95913-O-MOM-AVM B2a aglycone77.1>80>320
L-676,915AVM B2a aglycone>80>80
L-699,6184"-O-glucosyl AVM B1a160.0160
L-685,8694"-Deoxy-4"-epi-acetylamino-AVM B1a 5-ketoxime>160

Historical LD50 data are shown for comparison.

  • AVM, avermectin; IVM, 22,23-dihydro-avermectin; MEM, methoxyethoxymethyl; MOM, methoxymethyl; MeO, methoxy; MED, minimum effective dose.